Acetamide Scanning around Bicyclic Thiazoles: SAR at the H3 Receptor (pages 1559–1565)
Dr. Frédéric Denonne , Dr. Sylvain Célanire, Dr. Bernard Christophe, Sabine Defays, Christel Delaunoy, Dr. Marie-Laure Delporte, Dr. Eric Detrait, Véronique Durieu, Dr. Michel Gillard, Dr. Yves Lamberty, Dr. Geneviève Lorent, Jean-Marie Nicolas, Alain Vanbellinghen, Nathalie Van Houtvin and Dr. Laurent Provins
Article first published online: 14 JUL 2011 | DOI: 10.1002/cmdc.201100248
A surprisingly homogeneous SAR against the H3 receptor was revealed for positional acetamide isomers of bicyclic thiazoles fused to various cyclic amines. Pyrroline and azepine rings were used to probe the central position of the amide. In vitro ADMET parameters were measured, and the isomer with the best overall properties was assessed in vivo.